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BRPI0000908B8 - 4-phenyl-pyridine derivatives, their preparation process and their use, as well as the drug containing them - Google Patents

4-phenyl-pyridine derivatives, their preparation process and their use, as well as the drug containing them

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Publication number
BRPI0000908B8
BRPI0000908B8 BRPI0000908A BR0000908A BRPI0000908B8 BR PI0000908 B8 BRPI0000908 B8 BR PI0000908B8 BR PI0000908 A BRPI0000908 A BR PI0000908A BR 0000908 A BR0000908 A BR 0000908A BR PI0000908 B8 BRPI0000908 B8 BR PI0000908B8
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BR
Brazil
Prior art keywords
lower alkyl
hydrogen
phenyl
group
halogen
Prior art date
Application number
BRPI0000908A
Other languages
Portuguese (pt)
Other versions
BR0000908A (en
BR0000908B1 (en
Inventor
Galley Guido
Stadler Heinz
Boes Michael
Schnider Patrick
Branca Quirico
Godel Thierry
Hoffmann Torsten
Hunkeler Walter
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of BR0000908A publication Critical patent/BR0000908A/en
Publication of BR0000908B1 publication Critical patent/BR0000908B1/en
Publication of BRPI0000908B8 publication Critical patent/BRPI0000908B8/en

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Abstract

patente de invenção: <b>"derivados do 4-fenil-piridina"<d>. a presente invenção refere-se a compostos da fórmula geral em que r é hidrogênio, alquila inferior, alcóxi inferior, halogênio ou trifluorometila; r¹ é hidrogênio ou halogênio; ou r e r¹ podem ser juntos -ch=ch-ch=ch-; r² e r^ 2'^ são de modo independente um do outro hidrogênio, halogênio, trifluorometila, alcóxi inferior ou ciano; ou r² e r^ 2'^ podem ser juntos -ch=ch-ch=ch-, substituídos opcionalmente por um ou dois substituintes selecionados entre alquila inferior ou alcóxi inferior; r³ é hidrogênio, alquila inferior ou forma um grupamento cicloalquil; r^ 4^ é hidrogênio, -n(r^ 5^)~ 2~, -n(r^ 5^)(ch~ 2~)~ n~oh, -n(r^ 5^)s(o)~ 2~-alquila inferior, -n(r^ 5^)s(o)~ 2~-fenil, -n=ch-n(r^ 5^)~ 2~, -n(r^ 5^)c(o)r^ 5^ ou uma amina terciária cíclica do grupamento ou o grupamento r^ 5^ é, de modo independente um do outro, hidrogênio, c~ 3 - 6~-cicloalquila, benzila ou alquila inferior; r^ 6^ é hidrogênio, hidróxi, alquila inferior, -(ch~ 2~)~ n~coo-alquila inferior, -n(r^ 5^)co-alquila inferior, hidróxi-alquila inferior, ciano, -(ch~ 2~)~ n~o(ch~ 2~)~ n~oh, -cho ou um grupamento heterocíclico de 5 ou 6 membros, ligado opcionalmente por um grupamento alquileno, x é - c(o)n(r^ 5^)-, -(ch~ 2~)~ m~o-, -(ch~ 2~)~ m~n(r^ 5^)-, -n(r^ 5^)c(o)-, ou -n(r^ 5^)(ch~ 2~)~ m~-; n é 0 - 4; e m é 1 ou 2; e a sais de adição de ácido farmaceuticamente aceitáveis dos mesmos. os compostos de fórmula i apresentam uma alta afinidade para o receptor nk-1. podem ser usados para o tratamento de doenças, as quais refere-sem a antagonistas receptores de nk-1.patent: <b>"derivatives of 4-phenyl-pyridine" <d>. the present invention relates to compounds of the general formula wherein r is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; r¹ is hydrogen or halogen; or r and r¹ can be together -ch=ch-ch=ch-; R2 and R2' are independently of one another hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; or R2 and R2' can be together -ch=ch-ch=ch-, optionally substituted by one or two substituents selected from lower alkyl or lower alkoxy; r³ is hydrogen, lower alkyl or forms a cycloalkyl group; r4 is hydrogen, -n(r5c)2 2, -n(r5c)(ch2)n oh, -n(r5c)s(o) ~ 2-lower alkyl, -n(R^ 5^)s(o)~ 2-phenyl, -n=ch-n(R5^)~ 2~, -n(R^5^)c (O)R5 or a tertiary cyclic amine of the group or the R5 group is, independently of one another, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R6 is hydrogen, hydroxy, lower alkyl, -(CH2)-n-coo-lower alkyl, -n(R5)co-lower alkyl, hydroxy-lower alkyl, cyano, -(ch ~ 2~)~ n~o(ch~2~)~ n~oh, -cho or a 5- or 6-membered heterocyclic group, optionally linked by an alkylene group, x is -c(o)n(r~5 ^)-, -(ch~ 2~)~ m~o-, -(ch~2~)~ m~n(r^5^)-, -n(r^5^)c(o)-, or -n(R^5^)(C~2~)~m~-; n is 0 - 4; and m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. the compounds of formula I have a high affinity for the nk-1 receptor. can be used for the treatment of diseases, which refer to nk-1 receptor antagonists.

BRPI0000908A 1999-02-24 2000-02-23 4-phenyl-pyridine derivatives, their preparation process and their use, as well as the drug containing them BRPI0000908B8 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP99103504 1999-02-24
EP99123689 1999-11-29

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BR0000908A BR0000908A (en) 2000-09-12
BR0000908B1 BR0000908B1 (en) 2013-09-24
BRPI0000908B8 true BRPI0000908B8 (en) 2021-05-25

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